Back to Search
Start Over
Synthesis and Evaluation of Quinone Derivatives for Activity against Trypanosome cruzi.
- Source :
-
Chemical & pharmaceutical bulletin [Chem Pharm Bull (Tokyo)] 2021; Vol. 69 (12), pp. 1195-1199. - Publication Year :
- 2021
-
Abstract
- A series of quinone derivatives with a variety of side chains were synthesized. These synthetic quinone compounds were evaluated for in vitro antitrypanosomal activity against trypomastigotes and amastigotes of Trypanosoma cruzi, the causative agent of Chagas disease. Measurement of solubility of quinones and their ability to permeate cell membranes were assessed to address their possible use as oral drugs. Some synthesized compounds exhibited potent antitrypanosomal activity. However, most compounds with a promising activity showed poor solubility that did not seem suitable for oral usage. Meanwhile, compound 5a, an N-tert-butoxycarbonylpiperidine derivative, exhibited good antitrypanosomal activity, ability to permeate membranes, and good solubility.
Details
- Language :
- English
- ISSN :
- 1347-5223
- Volume :
- 69
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Chemical & pharmaceutical bulletin
- Publication Type :
- Academic Journal
- Accession number :
- 34853286
- Full Text :
- https://doi.org/10.1248/cpb.c21-00732